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Enhancing the therapeutic effect of 2-211At-astato-α-methyl-L-phenylalanine with probenecid loading
https://repo.qst.go.jp/records/84714
https://repo.qst.go.jp/records/8471426e4926b-6db9-44db-8d00-7c7fb2c3d30f
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-09-15 | |||||
| タイトル | ||||||
| タイトル | Enhancing the therapeutic effect of 2-211At-astato-α-methyl-L-phenylalanine with probenecid loading | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Hirofumi, Hanaoka
× Hirofumi, Hanaoka× Yasuhiro, Oshima× Hiroyuki, Suzuki× Ichiro, Sasaki× Tadashi, Watabe× Kazuhiro, Ooe× Shigeki, Watanabe× Noriko, Ishioka× Yasuhiro, Oshima× Ichiro, Sasaki× Shigeki, Watanabe× Noriko, Ishioka |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | L-type amino acid transporter 1 (LAT1) might be a useful target for tumor therapy, since it is highly expressed in various types of cancers. We previously developed an astatine-211 (211At)-labeled amino acid derivative, 2-[211At]-astato-α-methyl-L-phenylalanine (2-[211At]-AAMP), and demonstrated its therapeutic potential for LAT1-positive cancers. However, the therapeutic effect of 2-[211At]-AAMP was insufficient, probably due to its low tumor retention. The preloading of probenecid, an organic anion transporter inhibitor, can delay the clearance of some amino acid tracers from the blood and consequently increase their accumulation in tumors. In this study, we evaluated the effect of probenecid preloading on the biodistribution and therapeutic effect of 2-[211At]-AAMP in mice. In biodistribution studies, the blood radioactivity of 2-[211At]-AAMP significantly increased with probenecid preloading. Consequently, the accumulation of 2-[211At-AAMP] in tumors was significantly higher with probenecid than without probenecid loading. In a therapeutic study, tumor growth was suppressed by 2-[211At]-AAMP with probenecid, and the tumor volume was significantly lower in the treatment group than in the untreated control group from day 2 to day 30 (end of the follow-up period) after treatment. These results indicate that probenecid loading could improve the therapeutic effect of 2-[211At]-AAMP by increasing its accumulation in tumors. | |||||
| 書誌情報 |
Cancers 巻 13, 号 21, p. 5514, 発行日 2021-11 |
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| 出版者 | ||||||
| 出版者 | MDPI | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 2072-6694 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.3390/cancers13215514 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://www.mdpi.com/2072-6694/13/21/5514 | |||||
